NDLI: Berry and Citrus Phenolic Compounds Inhibit Dipeptidyl Peptidase IV: Implications in Diabetes Management

Content Provider	PubMed Central
Author	Fan, Junfeng Johnson, Michelle H. Lila, Mary Ann Yousef, Gad Mejia, Elvira Gonzalez De
Copyright Year	2013
Abstract	Beneficial health effects of fruits and vegetables in the diet have been attributed to their high flavonoid content. Dipeptidyl peptidase IV (DPP-IV) is a serine aminopeptidase that is a novel target for type 2 diabetes therapy due to its incretin hormone regulatory effects. In this study, well-characterized anthocyanins (ANC) isolated from berry wine blends and twenty-seven other phenolic compounds commonly present in citrus, berry, grape, and soybean, were individually investigated for their inhibitory effects on DPP-IV by using a luminescence assay and computational modeling. ANC from blueberry-blackberry wine blends strongly inhibited DPP-IV activity (IC50, 0.07 ± 0.02 to >300 μ M). Of the twenty-seven phenolics tested, the most potent DPP-IV inhibitors were resveratrol (IC50, 0.6 ± 0.4 nM), luteolin (0.12 ± 0.01 μ M), apigenin (0.14 ± 0.02 μ M), and flavone (0.17 ± 0.01 μ M), with IC50 values lower than diprotin A (4.21 ± 2.01 μ M), a reference standard inhibitory compound. Analyses of computational modeling showed that resveratrol and flavone were competitive inhibitors which could dock directly into all three active sites of DPP-IV, while luteolin and apigenin docked in a noncompetitive manner. Hydrogen bonding was the main binding mode of all tested phenolic compounds with DPP-IV. These results indicate that flavonoids, particularly luteolin, apigenin, and flavone, and the stilbenoid resveratrol can act as naturally occurring DPP-IV inhibitors.
Related Links	http://dx.doi.org/10.1155/2013/479505
Starting Page	479505
File Format	PDF
ISSN	1741427X
e-ISSN	17414288
Journal	Evidence-based Complementary and Alternative Medicine : eCAM
Volume Number	2013
Language	English
Publisher	Hindawi Publishing Corporation
Publisher Date	2013-01-01
Access Restriction	Open
Rights Holder	Hindawi Publishing Corporation
Subject Keyword	Complementary and alternative medicine Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Complementary and Alternative Medicine

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